title: Ophthalmic delivery of brinzolamide by liquid crystalline nanoparticles: in vitro and in vivo evaluation.
abstract: Brinzolamide (BLZ) is a drug used to treat glaucoma; however, its use is restricted due to some unwanted adverse events. The goal of this study was to develop BLZ-loaded liquid crystalline nanoparticles (BLZ LCNPs) and to figure out the possibility of LCNPs as a new therapeutic system for glaucoma. BLZ LCNPs were produced by a modified emulsification method and their physicochemical aspects were estimated. In vitro release study revealed BLZ LCNPs displayed to some extent prolonged drug release behavior in contrast to that of BLZ commercial product (Azopt®). The ex vivo apparent permeability coefficient of BLZ LCNP systems demonstrated a 3.47-fold increase compared with that of Azopt®. The pharmacodynamics was checked over by calculating the percentage fall in intraocular pressure and the pharmacodynamic test showed that BLZ LCNPs had better therapeutic potential than Azopt®. Furthermore, the in vivo ophthalmic irritation was evaluated by Draize test. In conclusion, BLZ LCNPs would be a promising delivery system used for the treatment of glaucoma, with advantages such as lower doses but maintaining the effectiveness, better ocular bioavailability, and patient compliance compared with Azopt®.
authors.affiliation: School of Pharmacy, Nanjing Medical University, Lane 818, East Tianyuan Road, Nanjing, Jiangsu, 211166, People's Republic of China.
authors.forename: Weijun
authors.initials: W
authors.lastname: Wu
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.forename: Lin
authors.initials: L
authors.lastname: Wu
authors.forename: Baoyan
authors.initials: B
authors.lastname: Wang
authors.forename: Zhongyuan
authors.initials: Z
authors.lastname: Wang
authors.forename: Qunwei
authors.initials: Q
authors.lastname: Xu
authors.forename: Hongliang
authors.initials: H
authors.lastname: Xin
mesh_terms: D060433:Administration, Ophthalmic; D000818:Animals; D002257:Carbonic Anhydrase Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D003315:Cornea / Q000378:metabolism; D003460:Crystallization; D066298:In Vitro Techniques; D007429:Intraocular Pressure / Q000187:drug effects; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D011817:Rabbits; D053838:Scattering, Small Angle; D013449:Sulfonamides / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D013843:Thiazines / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D013449:Sulfonamides; D013843:Thiazines; C111827:brinzolamide